盐酸阿米替林壳聚糖微球的制备及其载药性能

PREPARATION OF AMITRIPTYLINE HYDROCHLORIDE-CHITOSAN MICRO SPHERES AND STUDY OF THEIR DRUG-RELEASING PERFORMANCES

以一种三环类抗抑郁药盐酸阿米替林为模型药物,采用乳化分散-化学交联法,以乙二醇二缩水甘油醚(ethylene glycol diglycidyl ether,EGDE)为交联剂,制备了盐酸阿米替林壳聚糖微球,考察了其理化性质和释放性能.EGDE两末端为环氧基团,与氨基反应生成-C-N-键从而起交联作用.所得微球球形规整,呈乳白色,释药速率随CS浓度增大而减慢,在酸性缓冲溶液中略大于碱性缓冲溶液中.研究结果表明盐酸阿米替林-壳聚糖微球具有较好的药物缓释性能.

By using Amitriptyline Hydrochloride as the model drug, amitriptyline hydrochlo- ride -chitosan microspheres were prepared by emulsion cross -linking techniques with eth- ylene glycol diglycidyl ether （EGDE） as a cross -linking agent. The physicochemical properties and the drug - release performances of the microspheres were investigated. EGDE has epoxy groups and cross - linking reaction occurred with the groups of - NH2 on CS. The microspheres have the color of white, a spherical shape and an average diameter about 12.32 μm. The drug loaded efficiency is 26.25% and the content of the drug is 6.56% （ω/ω）. With the increase of the concentration of CS, the releasing ratio of Amitriptyline Hydrochloride decreases. The result indicated that the mierospheres have a satisfactory performance of slowly releasing the drug of Amitriptyline Hydrochloride.